Bromocriptine
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Bromocriptine is an antiparkinson and antidiabetic drug that works by stimulating dopamine receptors in the brain. It is also used to treat hyperprolactinemia and acromegaly. It has a rapid onset of around 1-2 hours, is highly protein bound, and primarily metabolized by the liver via CYP3A4 enzymes. Common side effects include dizziness, nausea, and hypotension. It can interact with other drugs that are CYP3A4 inhibitors or substrates, as well as ergot alkaloids, dopamine antagonists, and medications with vasoconstrictive effects. Initial dosing is usually at bedtime to reduce potential central nervous system side effects
Bromocriptine
- 1. Bromocriptine Trade name: parlodel Class: Antiparkinson agent
- 2. Dosage form available Tablet :1 mg,2.5 mg. Capsule : 5 mg ,10 mg .
- 3. Pharmacology Stimulates dopamine receptors in brain, relieving parkinsonian symptoms . Inhibits prolactin, which is responsible for lactation, and lowers elevated blood levels of growth hormone in acromegaly . The mechanism in glycemic control is unknown..
- 4. Pharmacokinetic data 1-2 h Onset Major elimination route is hepatic; 6% is renally eliminated . Terminal half - life of 15 h Elimination Primarily metabolized in the GI tract and liver ( CYP3A4 ). Undergoes extensive first - pass metabolism Metabolism to 96% bound to serum albumin 90 Distribution of oral dose absorbed 28% Absorption
- 5. Indications and Usage *Treatment of hyperprolactinemia-associated disorders (eg, amenorrhea with or without galactorrhea, infertility, hypogonadism). *in patients with prolactin-secreting adenomas * treatment of acromegaly *therapy for Parkinson disease (idiopathic or postencephalitic) *therapy for type 2 diabetes
- 6. Dose 1- Prevention or suppression of lactation 2.5 mg on day 1 (prevention) or daily for 2–3 days (suppression); then 2.5 mg twice daily for 14 days 2-Hypogonadism, galactorrhoea, infertility , initially 1–1.25 mg at bedtime, increased gradually; usual dose 7.5 mg daily in divided doses, increased if necessary to max. 30 mg daily, usual dose in infertility without hyperprolactinaemia, 2.5 mg twice daily.
- 7. 3-Acromegaly , initially 1–1.25 mg at bedtime, increase gradually to 5 mg every 6 hours 4-Prolactinoma, initially 1–1.25 mg at bedtime; increased gradually to 5 mg every 6 hours (occasional patients may require up to 30 mg daily) 5- child under 15 years, not recommended
- 8. Contraindications * Hypersensitivity to bromocriptine, ergot alkaloids or ergot - related drugs, or any component of the product; breast - feeding.. *They should also be avoided in pre - eclampsia *Uncontrolled hypertension; pregnancy postpartum period in women with a history of coronary artery disease or severe CV conditions
- 9. Adverse Reactions Cardiovascular Postural / orthostatic hypotension , syncope ,cardiac valvulopathy, hypertension, MI, stroke CNS Headache, dizziness , fatigue , light - headedness , somnolence ,drowsiness ,confusion, hallucinations, psychomotor agitation, psychotic disorders, seizures EENT Rhinitis , sinusitis ,amblyopia dry mouth / nasal stuffiness
- 10. Metabolic Hypoglycemia Respiratory Constrictive pericarditis, pleural and pericardial effusion, pleural and pulmonary fibrosis, pleural thickening GI Nausea , constipation , diarrhea ,dyspepsia , vomiting anorexia ,abdominal cramps , GI bleeding
- 11. Drugs ineraction CYP3A4 strong inhibitors (eg, azole antifungals, protease inhibitors ) Pharmacologic and toxic effects of bromocriptine may beincreased. Coadminister with caution Dopamine antagonists (eg, butyrophenones, metoclopramide, phenothiazine Dopamine antagonists may reduce bromocriptine efficacy; bromocriptine may reduce effectiveness of dopamine antagonists. Concurrent use is not recommended
- 12. Ergot drugs (eg, ergotamine) Coadministration may increase occurrence of ergot-related side effects (eg, fatigue, nausea, vomiting) and may reduce effectiveness of ergot drugs when used to treat migraines. Concomitant use is not recommended . Erythromycin, octreotide May increase bromocriptine serum levels Ethanol May potentiate adverse effects of bromocriptine
- 13. Highly protein—bound drugs (eg, chloramphenicol, probenecid, salicylates, sulfonamides) Bromocriptine may increase the unbound fraction of other concomitantly used highly protein—bound drugs Methyldopa Hypotensive effects may be increased Triptans (eg, sumatriptan May have additive vasoconstrictive effects. Avoid concomitant use
- 14. General Advice ** Give with milk or meals to reduce gastric distress…… **Initial dose of Parlodel is usually given at bedtime because of adverse CNS reactions ( eg, dizziness, fainting).